Pub Date : 2019-10-24DOI: 10.2174/2213335606666190724093305
N. Patel, Sabir S Pathan, Hetal I. Soni
For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation.The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds.Microwave irradiation was used for the synthesis of 2-((3-cyano-4-(3,4-dichloro phenyl)- 6-(4-hydroxy-3-methoxyphenyl) pyridin-2-yl) amino)-N-(5-(substituted) -(6-methyl-2-oxo -1,2,3,4- tetrahydro pyrimidin-5-yl)-1,3,4-oxadiazol-2-yl)acetamide by using Biginelli reaction. New structural analogues were confirmed by spectral studies followed by their screening for in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus Pyogenus, Escherichia coli and Pseudomonas aeruginosa bacterial strains and for antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity determined out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium.As compared to the conventional method, microwave irradiation method is advantageous for the synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antitubercular activity were found for some of the compounds.Microwave irradiation method provided an effective way to discover a novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.
{"title":"3,4-Dihydropyrimidin-2(1H)-One Analogues: Microwave irradiated Synthesis with Antimicrobial and Antituberculosis Study","authors":"N. Patel, Sabir S Pathan, Hetal I. Soni","doi":"10.2174/2213335606666190724093305","DOIUrl":"https://doi.org/10.2174/2213335606666190724093305","url":null,"abstract":"For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation.The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds.Microwave irradiation was used for the synthesis of 2-((3-cyano-4-(3,4-dichloro phenyl)- 6-(4-hydroxy-3-methoxyphenyl) pyridin-2-yl) amino)-N-(5-(substituted) -(6-methyl-2-oxo -1,2,3,4- tetrahydro pyrimidin-5-yl)-1,3,4-oxadiazol-2-yl)acetamide by using Biginelli reaction. New structural analogues were confirmed by spectral studies followed by their screening for in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus Pyogenus, Escherichia coli and Pseudomonas aeruginosa bacterial strains and for antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity determined out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium.As compared to the conventional method, microwave irradiation method is advantageous for the synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antitubercular activity were found for some of the compounds.Microwave irradiation method provided an effective way to discover a novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2213335606666190724093305","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42213575","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-24DOI: 10.2174/2213335606666190820091029
Prashant B. Hiremath and Kantharaju Kamanna
The agricultural wastes as a source offer an excellent alternative to replace many toxic and environmentally hazardous catalysts, due to their least toxicity, ease of biodegradability, and ability to act as a greener catalytic medium. Some of the agro-waste based catalysts reported are BFE, WERSA, WEB, and WEPBA. 2-Amino-4H-chromene derivatives are promising biologically potent heterocyclic compounds, due to their medicinal applications such as antimicrobial, anti-inflammatory, antibacterial, antiviral, anticancer, antidiuretic, anticoagulant and antianaphylactic activities. The present work describes a microwave accelerated, efficient, eco-friendly and economical approach for the synthesis of 2-amino-4H-chromenes through condensation of substituted arylaldehyde, malononitrile and resorcinol/naphthol catalyzed water extract of pomegranate peel ash (WEPPA) under microwave irradiation. The reaction completed within 3-6 min with good to excellent yield of product isolation. The final product isolated by simple filtration and recrystallization gave a spectroscopically pure form of product and did not require further purification.The pomegranate peel ash water extract as an agro-waste derived catalyst was employed under microwave irradiation for the economical synthesis of 2-amino-4H-chromene derivatives.The reported agro-waste based catalyst was obtained in the absence of external base, additives and solvent-free synthesis of 2-amino-4H-chromene using aryl aldehyde, malononitrile and resorcinol/ naphthol under microwave irradiation. WEPPA acts as a solvent media and catalyst, as it plays a dual role in the synthesis of 2-amino-4H-chromenes.We established an efficient, simple, agro-waste based catalytic approach for the synthesis of 2-amino-4H-chromene derivatives from the condensation of arylaldehyde, malononitrile and resorcinol/α-naphthol/β-naphthol employing WEPPA as an efficient catalyst under microwave synthesis. The method has found to be a greener, economic and eco-friendly approach for the synthesis of chromene scaffolds. The advantages of the present approach are solvent-free, no external metal, chemical base free, short reaction time and isolated product in good to excellent yields. The catalyst is agro-waste derived, which has abundant natural sources available, thus making the present approach a greener one.
{"title":"A Microwave Accelerated Sustainable Approach for the Synthesis of 2-amino-4H-chromenes Catalysed by WEPPA: A Green Strategy","authors":"Prashant B. Hiremath and Kantharaju Kamanna","doi":"10.2174/2213335606666190820091029","DOIUrl":"https://doi.org/10.2174/2213335606666190820091029","url":null,"abstract":"The agricultural wastes as a source offer an excellent alternative to replace many toxic and environmentally hazardous catalysts, due to their least toxicity, ease of biodegradability, and ability to act as a greener catalytic medium. Some of the agro-waste based catalysts reported are BFE, WERSA, WEB, and WEPBA. 2-Amino-4H-chromene derivatives are promising biologically potent heterocyclic compounds, due to their medicinal applications such as antimicrobial, anti-inflammatory, antibacterial, antiviral, anticancer, antidiuretic, anticoagulant and antianaphylactic activities. The present work describes a microwave accelerated, efficient, eco-friendly and economical approach for the synthesis of 2-amino-4H-chromenes through condensation of substituted arylaldehyde, malononitrile and resorcinol/naphthol catalyzed water extract of pomegranate peel ash (WEPPA) under microwave irradiation. The reaction completed within 3-6 min with good to excellent yield of product isolation. The final product isolated by simple filtration and recrystallization gave a spectroscopically pure form of product and did not require further purification.The pomegranate peel ash water extract as an agro-waste derived catalyst was employed under microwave irradiation for the economical synthesis of 2-amino-4H-chromene derivatives.The reported agro-waste based catalyst was obtained in the absence of external base, additives and solvent-free synthesis of 2-amino-4H-chromene using aryl aldehyde, malononitrile and resorcinol/ naphthol under microwave irradiation. WEPPA acts as a solvent media and catalyst, as it plays a dual role in the synthesis of 2-amino-4H-chromenes.We established an efficient, simple, agro-waste based catalytic approach for the synthesis of 2-amino-4H-chromene derivatives from the condensation of arylaldehyde, malononitrile and resorcinol/α-naphthol/β-naphthol employing WEPPA as an efficient catalyst under microwave synthesis. The method has found to be a greener, economic and eco-friendly approach for the synthesis of chromene scaffolds. The advantages of the present approach are solvent-free, no external metal, chemical base free, short reaction time and isolated product in good to excellent yields. The catalyst is agro-waste derived, which has abundant natural sources available, thus making the present approach a greener one.","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2213335606666190820091029","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42259164","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-24DOI: 10.2174/2213335606666190906123431
D. E. Jimenez, L. L. Zanin, L. F. Diniz, J. Ellena, A. Porto
The Knoevenagel condensation is an important reaction in organic chemistry because of its capacity to form new C-C bonds and its products are mainly used in organic synthesis as intermediates, due to the large number of reactions they can undergo. Based on the importance of the Knoevenagel adducts, a sustainable synthetic methodology was developed employing microwave irradiation. Develop a synthetic methodology employing microwave irradiation and green solvents to obtain Knoevenagel adducts with high yields. Knoevenagel condensation reactions were evaluated with different basic catalysts, as well as in the presence or absence of microwave irradiation. The scope of the reaction was expanded using different aldehydes, cyanoacetamide or methyl cyanoacetate. The geometry of the formed products was also evaluated. After the optimization process, the reactions between aldehydes and cyanoacetamide were performed with triethylamine as catalyst, in the presence of microwave irradiation, in 35 minutes, using NaCl solution as solvent and resulted in high yields 90-99%. The reactions performed between aldehydes and methyl cyanoacetate were also performed under these conditions, but showed better yields with EtOH as solvent 70-90%. Finally, from X-ray analysis, the (E)-geometry of these compounds was confirmed. In this study we developed synthetic methodology of Knoevenagel condensation using triethylamine, green solvents and microwave irradiation. In 35 minutes, products with high yields (70- 99%) were obtained and the (E)-geometry of the adducts was confirmed.
{"title":"Green Synthetic Methodology of (E)-2-cyano-3-aryl Selective Knoevenagel Adducts Under Microwave Irradiation","authors":"D. E. Jimenez, L. L. Zanin, L. F. Diniz, J. Ellena, A. Porto","doi":"10.2174/2213335606666190906123431","DOIUrl":"https://doi.org/10.2174/2213335606666190906123431","url":null,"abstract":"\u0000\u0000The Knoevenagel condensation is an important reaction in organic chemistry\u0000because of its capacity to form new C-C bonds and its products are mainly used in organic synthesis as\u0000intermediates, due to the large number of reactions they can undergo. Based on the importance of the\u0000Knoevenagel adducts, a sustainable synthetic methodology was developed employing microwave irradiation.\u0000\u0000\u0000\u0000Develop a synthetic methodology employing microwave irradiation and green solvents to\u0000obtain Knoevenagel adducts with high yields.\u0000\u0000\u0000\u0000Knoevenagel condensation reactions were evaluated with different basic catalysts, as well as\u0000in the presence or absence of microwave irradiation. The scope of the reaction was expanded using\u0000different aldehydes, cyanoacetamide or methyl cyanoacetate. The geometry of the formed products\u0000was also evaluated.\u0000\u0000\u0000\u0000After the optimization process, the reactions between aldehydes and cyanoacetamide were\u0000performed with triethylamine as catalyst, in the presence of microwave irradiation, in 35 minutes, using\u0000NaCl solution as solvent and resulted in high yields 90-99%. The reactions performed between\u0000aldehydes and methyl cyanoacetate were also performed under these conditions, but showed better\u0000yields with EtOH as solvent 70-90%. Finally, from X-ray analysis, the (E)-geometry of these compounds\u0000was confirmed.\u0000\u0000\u0000\u0000In this study we developed synthetic methodology of Knoevenagel condensation using\u0000triethylamine, green solvents and microwave irradiation. In 35 minutes, products with high yields (70-\u000099%) were obtained and the (E)-geometry of the adducts was confirmed.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2213335606666190906123431","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48590610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-24DOI: 10.2174/2213335606666190307162901
H. Badwaik, A. Alexander, Kalyani Sakure
Nowadays, microwave assisted techniques are becoming popular ecofriendly approaches in Green Chemistry. However, to date, no study has reported the microwave assisted graft copolymerization of acrylamide on carboxymethyl xanthan gum backbone. The objective of this study was to study the effect of microwave radiations on graft copolymerization of acrylamide on carboxymethyl xanthan gum. Carboxymethyl xanthan gum was grafted with acrylamide under microwave irradiation. The grafting process is optimized by varying the amount of carboxymethyl xanthan gum, acrylamide, ammonium persulphate, microwave power and exposure time. The graft copolymer was further characterized and evaluated for its efficacy. Grafting was successfully optimized for higher grafting efficiency (92.4 %) and grafting (410.5 %) in a short reaction time of 150 s, at 40 times less concentration of ammonium persulphate. The characterization study confirmed the grafting of acrylamide on the hydroxyl group of carboxymethyl xanthan gum backbone. Microwave radiations play a vital role in graft copolymerization of acrylamide on carboxymethyl xanthan gum, in short reaction time, at 40 times less concentration of initiator. The synthesized graft copolymers remain nontoxic and also showed more antimicrobial activity than carboxymethyl xanthan gum.
{"title":"Understanding the Significance of Microwave Radiation for the Graft Copolymerization of Acrylamide on Carboxymethyl Xanthan Gum","authors":"H. Badwaik, A. Alexander, Kalyani Sakure","doi":"10.2174/2213335606666190307162901","DOIUrl":"https://doi.org/10.2174/2213335606666190307162901","url":null,"abstract":"\u0000\u0000Nowadays, microwave assisted techniques are becoming popular ecofriendly\u0000approaches in Green Chemistry. However, to date, no study has reported the microwave assisted\u0000graft copolymerization of acrylamide on carboxymethyl xanthan gum backbone.\u0000\u0000\u0000\u0000The objective of this study was to study the effect of microwave radiations on graft copolymerization\u0000of acrylamide on carboxymethyl xanthan gum.\u0000\u0000\u0000\u0000Carboxymethyl xanthan gum was grafted with acrylamide under microwave irradiation.\u0000The grafting process is optimized by varying the amount of carboxymethyl xanthan gum, acrylamide,\u0000ammonium persulphate, microwave power and exposure time. The graft copolymer was further characterized\u0000and evaluated for its efficacy.\u0000\u0000\u0000\u0000Grafting was successfully optimized for higher grafting efficiency (92.4 %) and grafting\u0000(410.5 %) in a short reaction time of 150 s, at 40 times less concentration of ammonium persulphate.\u0000The characterization study confirmed the grafting of acrylamide on the hydroxyl group of carboxymethyl\u0000xanthan gum backbone.\u0000\u0000\u0000\u0000Microwave radiations play a vital role in graft copolymerization of acrylamide on carboxymethyl\u0000xanthan gum, in short reaction time, at 40 times less concentration of initiator. The synthesized\u0000graft copolymers remain nontoxic and also showed more antimicrobial activity than carboxymethyl\u0000xanthan gum.\u0000","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2213335606666190307162901","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48458456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-02-22DOI: 10.2174/2213335606666181122101724
B. Kahveci, E. Menteşe
{"title":"Microwave Assisted Synthesis of Coumarins: A Review From 2007 to 2018","authors":"B. Kahveci, E. Menteşe","doi":"10.2174/2213335606666181122101724","DOIUrl":"https://doi.org/10.2174/2213335606666181122101724","url":null,"abstract":"","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43107743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-02-22DOI: 10.2174/2213335606666190125161512
Santosh Y. Khatavi and Kamanna Kantharaju
{"title":"Microwave Accelerated Synthesis of 2-Oxo-2H-Chromene-3-Carboxylic Acid Using WELFSA","authors":"Santosh Y. Khatavi and Kamanna Kantharaju","doi":"10.2174/2213335606666190125161512","DOIUrl":"https://doi.org/10.2174/2213335606666190125161512","url":null,"abstract":"","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44913822","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-02-22DOI: 10.2174/2213335605666181024142317
Rakesh D. Amrutkar and Mahendra S. Ranawat
{"title":"Design, Microwave Assisted Organic Synthesis and Molecular Docking Studies of Some 4 - (3H)-Quinazolinone Derivatives as Inhibitors of Colchicine- Binding Site of Tubulin","authors":"Rakesh D. Amrutkar and Mahendra S. Ranawat","doi":"10.2174/2213335605666181024142317","DOIUrl":"https://doi.org/10.2174/2213335605666181024142317","url":null,"abstract":"","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41784513","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-01-18DOI: 10.2174/2213335606666190118161943
C. Nalini, S. Amuthalakshmi, V. S. Shanthanakrishnan
{"title":"Heterocyclic Derivatives: Easy Three-component Microwave assisted Synthesis, and Anticonvulsant, Anti inflammatory Evaluation","authors":"C. Nalini, S. Amuthalakshmi, V. S. Shanthanakrishnan","doi":"10.2174/2213335606666190118161943","DOIUrl":"https://doi.org/10.2174/2213335606666190118161943","url":null,"abstract":"","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2019-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45144060","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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